Fig. 1 · Structure
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Enitociclib
CDK9 Inhibitor
Enitociclib is a highly selective CDK9 inhibitor, with an IC50 value of 3 nM, that disrupts transcriptional elongation by inhibiting Ser2/Ser5 phosphorylation of RNA polymerase II. This compound specifically targets and depletes short-lived oncogenic proteins such as c-MYC and MCL-1, thereby inducing apoptosis in tumor cells. Enitociclib also impairs enhancer RNA production and enhancer-promoter interactions, leading to downregulation of oncogene expression at the epigenetic level. Its efficacy is demonstrated through synergistic interactions with agents like Bortezomib, Lenalidomide, Pomalidomide, Venetoclax, and Paclitaxel, providing a valuable research tool for studying malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma, and pancreatic ductal adenocarcinoma.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Inhibitor |
| CAS Number | 1610408-97-3 |
| Applications | CDK9 Inhibitor |
| Formula | C19H18F2N4O2S |
| Molecular Weight | 404.43 |
| Synonyms | (+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib |
| SMILES | COC1=C(C2=C(F)C=NC(NC3=CC(C[S@@](=O)(C)=N)=CC=N3)=C2)C=CC(F)=C1 |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.